Gepirone. Organon
by
Leslie R A.
Addenbrooke's Centre for Clinical Investigation,
Cambridge, UK.
Ron_Leslie-1@gsk.com
Curr Opin Investig Drugs 2001 Aug;2(8):1120-7


ABSTRACT

Gepirone, a pyridinyl piperazine 5-HT1A receptor agonist, has been developed by Fabre-Kramer as an antidepressant. Bristol-Myers Squibb (BMS) outlicensed the compound to Fabre-Kramer in 1993 and is no longer involved in its development [337393]. In May 1998, NV Organon (a subsidiary of Akzo Nobel) licensed the rights to the drug product for further development and marketing from Fabre-Kramer and, by October 1999, had submitted the drug for approval in the US [347133]. In December 2000, the company expected US and European launches in 2002 and 2003, respectively [402686]. Mechanism of action studies have demonstrated that gepirone, compared to buspirone, possesses a much greater selectivity for 5-HT1A receptors over dopamine D2 receptors. Long-term studies have shown that gepirone has a differential action at presynaptic (agonist) and post-synaptic (partial agonist) 5-HT1A receptors. However, further studies are still required to determine the relative contribution of pre- and post-synaptic 5-HT1A receptors to the therapeutic action of gepirone and related compounds. In March 2001, according to Schroder Salomon Smith Barney, Akzo Nobel targeted peak sales of Euro 300 million for gepirone [409013]. This amout was reiterated in an April 2001 report by HSBC Securities, which stated that gepirone was expected to achieve this figure in 2009 or 2010 [409014].
SSRIs
5-HT1a
F11440
Anxiety
Gepirone
Serotonin
Ipsapirone
Alprazolam
Adinazolam
Eltoprazine
Alnespirone
Benzodiazepines
Future anxiolytics
Gepirone: structure
Buspirone + pindolol
Virtual reality exposure
Neuropepide Y and anxiety
Gepirone: immediate v extended-release


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